Practical aspects of transporter model systems: a case study involving SQV.

abstract：:The body is considered as a system composed of a number of subsystems. The response(s) of a drug is a complicated function of the concentration in the blood plasma, which in turn is some function of the dosage input. The dose-response curve of a drug in a subsystem (e.g., isolated organ) is, over a limited concentrati...

journal_title：Drug metabolism reviews

authors： van Rossum JM,Burgers JP

更新日期：1984-01-01 00:00:00

abstract：:Numerous experimental and epidemiological studies have demonstrated that polycyclic aromatic hydrocarbons (PAHs), which are major constituents of cigarette tobacco tar, are strongly involved in the pathogenesis of the cardiovascular diseases (CVDs). Knowing that PAH-induced toxicities are mediated by the activation of...

journal_title：Drug metabolism reviews

authors： Korashy HM,El-Kadi AO

更新日期：2006-01-01 00:00:00

abstract：:Like any other drugs, antiallergic medications can be associated with large inter- and intraindividual variability in their disposition. The best-documented examples belong to the H1 antihistamines. Variable drugs are more likely to show unpredictable therapeutic response with both increased risks of side effects and ...

journal_title：Drug metabolism reviews

authors： Nicolas JM,Espie P,Molimard M

更新日期：2009-01-01 00:00:00

abstract：:1. The metabolic activity of the gastrointestinal microflora can be modified by numerous factors derived from the host, the host's environment, and the flora itself. 2. Marked differences exist in microbial composition and metabolism of the gut floras of different species of animal, and in the degree of colonization o...

journal_title：Drug metabolism reviews

authors： Rowland IR

更新日期：1988-01-01 00:00:00

abstract：:Glycyrrhizic acid is widely applied as a sweetener in food products and chewing tobacco. In addition, it is of clinical interest for possible treatment of chronic hepatitis C. In some highly exposed subjects, side effects such as hypertension and symptoms associated with electrolyte disturbances have been reported. To...

journal_title：Drug metabolism reviews

authors： Ploeger B,Mensinga T,Sips A,Seinen W,Meulenbelt J,DeJongh J

更新日期：2001-05-01 00:00:00

abstract：:Ronald Estabrook made his initial impact studying cytochrome P450 by demonstrating the oxidative metabolism function of this unique class of enzymes, which had an unusual spectral peak at 450 nm when reduced and in the presence of carbon monoxide. Utilizing a photochemical action spectrum, he demonstrated that a cytoc...

journal_title：Drug metabolism reviews

authors： Sheets JJ

更新日期：2007-01-01 00:00:00

abstract：:Cytochrome P450 (CYP) 2D6 is one of the most important enzymes involved in the metabolism of drugs. Multiple, clinically relevant, genetic variants of this gene have been identified and, among them, a gene deletion as well as multiplications of the gene. These large structural mutations in CYP2D6 occur at a relatively...

journal_title：Drug metabolism reviews

authors： Meijerman I,Sanderson LM,Smits PH,Beijnen JH,Schellens JH

更新日期：2007-01-01 00:00:00

abstract：:Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic releva...

journal_title：Drug metabolism reviews

authors： Dinis-Oliveira RJ

更新日期：2017-02-01 00:00:00

abstract：:Traditional Chinese medicine (TCM) has a long history of medical use in China and is still used worldwide. Unexpected herb-drug interactions (HDIs) may lead to adverse drug reactions or loss of therapeutic efficacy of the victim drug. Here, based on searches of Medline, EBSCO, Science Direct and Web of Science using v...

journal_title：Drug metabolism reviews

authors： Ma BL,Ma YM

更新日期：2016-01-01 00:00:00

abstract：:The physiological and biochemical measurements that can be performed noninvasively in humans with modern imaging techniques offer great promise for defining the precise state of a patient's disease and its response to therapy. In general, there are two critical points in drug development when PET measurements are like...

journal_title：Drug metabolism reviews

authors： Fischman AJ,Alpert NM,Babich JW,Rubin RH

更新日期：1997-11-01 00:00:00

abstract：:Flavin-containing monooxygenases (FMOs) are important oxidative drug metabolizing enzymes. FMO3 is the primary human adult liver FMO enzyme, but is developmentally regulated. FMO3 promoter characterization using in vitro DNA binding assays with HepG2 cell and fetal and adult liver nuclear protein, as well as FMO3/repo...

journal_title：Drug metabolism reviews

authors： Klick DE,Hines RN

更新日期：2007-01-01 00:00:00

abstract：:Indirect evidence for the participation of cytochrome P450 (P450) in the microsomal N-oxygenation of primary and N-substituted amine functions is presented by studies employing diagnostic modifiers of the hemoprotein system as well as immunochemical approaches. Experiments with recombinant hemoproteins or isozymes pur...

journal_title：Drug metabolism reviews

authors： Hlavica P

更新日期：2002-08-01 00:00:00

abstract：:Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). CYP1A2 is subject to rev...

journal_title：Drug metabolism reviews

authors： Zhou SF,Wang B,Yang LP,Liu JP

更新日期：2010-05-01 00:00:00

abstract：:Nano-hydroxyapatite (nano-HA) is a material with multiple uses due to its biocompatibility and its resemblance to the nonorganic bone structure. It is used in various dental domains such as implantology, surgery, periodontology, esthetics and prevention. The aim of this study is to provide a wide understanding of nano...

journal_title：Drug metabolism reviews

authors： Bordea IR,Candrea S,Alexescu GT,Bran S,Băciuț M,Băciuț G,Lucaciu O,Dinu CM,Todea DA

更新日期：2020-05-01 00:00:00

abstract：:In summary, the concerns that environmental and other agents are causing adverse effects on reproductive function in humans are real, although the risk is not necessarily well characterized. The range of concerns for the types of effect that agents might have on reproduction span the full range of reproductive events....

journal_title：Drug metabolism reviews

authors： Schwetz BA

更新日期：1996-02-01 00:00:00

abstract：:When target organ toxicity arises in animal models during routine drug safety evaluation, it raises several key questions: Is this target organ toxicity related to the pharmacology? What is the mode of action (MOA)? Is the target organ toxicity relevant to humans? Pathology or prior knowledge of the compound class may...

journal_title：Drug metabolism reviews

authors： Roberts R,Cain K,Coyle B,Freathy C,Leonard JF,Gautier JC

更新日期：2003-11-01 00:00:00

abstract：:Hyperbilirubinemia may accompany harmful effects such as jaundice, brain dysfunction, and pharmacokinetic alterations of drugs. Clinical drugs are the important causes of hyperbilirubinemia, especially for patients with certain pathologic conditions or with genetic variations. This article reviews hyperbilirubinemic p...

journal_title：Drug metabolism reviews

authors： Ah YM,Kim YM,Kim MJ,Choi YH,Park KH,Son IJ,Kim SG

更新日期：2008-01-01 00:00:00

abstract：:Mineral fibers, including asbestos, are ubiquitous contaminants of the environment. Asbestos fibers are generally present at levels below 1 fiber/L in air though 10 fibers/L may be found in cities; these levels do not appear to be high enough to present a hazard to health. These fibers come mostly from the use of fibr...

journal_title：Drug metabolism reviews

authors： Hoskins JA,Brown RC

更新日期：1994-01-01 00:00:00

abstract：:An association between marijuana use and schizophrenia has been noted for decades, and the recent emergence of high-efficacy synthetic cannabinoids (SCBs) as drugs of abuse has lead to a growing number of clinical reports of persistent psychotic effects in users of these substances. The mechanisms underlying SCB-elici...

journal_title：Drug metabolism reviews

authors： Fantegrossi WE,Wilson CD,Berquist MD

更新日期：2018-02-01 00:00:00

abstract：:The rat P450IIA subfamily was characterized at the protein, cDNA, and gene level. The purified IIA1 and IIA2 P-450s displayed distinct positional specificities toward hydroxylation of the prototype substrate testosterone. The IIA1 and IIA2 genes were also regulated differently during development; IIA1 was expressed wi...

journal_title：Drug metabolism reviews

authors： Gonzalez FJ,Matsunaga T,Nagata K

更新日期：1989-01-01 00:00:00

abstract：:The recent progresses in molecular biology and pharmacology approaches allowed the characterization of a series of nuclear receptors (NRs) as efficient regulators of uridine diphosphate glucuronosyltransferase (UGT) genes activity. These regulatory processes ensure an optimized UGT expression in response to specific e...

journal_title：Drug metabolism reviews

authors： Bigo C,Caron S,Dallaire-Théroux A,Barbier O

更新日期：2013-02-01 00:00:00

abstract：:The high rate of attrition during drug development and its associated high research and development (R&D) cost have put pressure on pharmaceutical companies to ensure that candidate drugs going to clinical testing have the appropriate quality such that the biological hypothesis could be evaluated. To help achieve this...

journal_title：Drug metabolism reviews

authors： Ballard P,Brassil P,Bui KH,Dolgos H,Petersson C,Tunek A,Webborn PJ

更新日期：2012-08-01 00:00:00

abstract：:The efficacy of drugs has to be demonstrated following the principal approach of statistical evaluation in controlled clinical trials. This scientifically and internationally accepted numerical approach has developed over the years to its importance, in contrast to the more pharmacologically attempt to extrapolate hum...

journal_title：Drug metabolism reviews

authors： Hildebrandt AG

更新日期：2004-10-01 00:00:00

abstract：:Glutathione S-transferase P1-1 (GSTP) is one member of the family of GSTs and is ubiquitously expressed in human tissues. The literature is replete with reports of high levels of GSTP linked either with cancer incidence or drug resistance, and yet no entirely cogent explanation for these correlations exists. The catal...

journal_title：Drug metabolism reviews

authors： Tew KD,Townsend DM

更新日期：2011-05-01 00:00:00

abstract：:Global statistical data shed light on an alarming trend that every year thousands of people die due to adverse drug reactions as each individual responds in a different way to the same drug. Pharmacogenomics has come up as a promising field in drug development and clinical medication in the past few decades. It has em...

journal_title：Drug metabolism reviews

authors： Chaudhary R,Singh B,Kumar M,Gakhar SK,Saini AK,Parmar VS,Chhillar AK

更新日期：2015-08-01 00:00:00

abstract：:Chemicals that cause toxicity though a direct mechanism, such as acetaminophen, covalently bind to a select group of proteins prior to the development of toxicity, and these proteins may be important in the initiation of the events that lead to the hepatotoxicity. Disruption of the cell is measured by release of intra...

journal_title：Drug metabolism reviews

authors： Pumford NR,Halmes NC,Hinson JA

更新日期：1997-02-01 00:00:00

abstract：:Synthetic cannabinoids (SC), originally developed as research tools, are now highly abused novel psychoactive substances. We present a comprehensive systematic review covering in vivo and in vitro animal and human pharmacokinetics and analytical methods for identifying SC and their metabolites in biological matrices. ...

journal_title：Drug metabolism reviews

authors： Castaneto MS,Wohlfarth A,Desrosiers NA,Hartman RL,Gorelick DA,Huestis MA

更新日期：2015-05-01 00:00:00

abstract：:S-carboxymethyl-L-cysteine, the side-chain carboxymethyl derivative of the sulfur-containing amino acid, cysteine, has been known and available for almost 80 years. During this time, it has been put to a variety of uses, but it is within the field of respiratory medicine that, presently, it has found a clinical niche....

journal_title：Drug metabolism reviews

authors： Mitchell SC,Steventon GB

更新日期：2012-05-01 00:00:00

abstract：:By inhibiting ACE, captopril blocks the conversion of AI or AII and augments the effects of bradykinin both in vitro and in vivo. In rats, dogs, and monkeys with 2-kidney renal hypertension, orally administered captopril rapidly and markedly reduces blood pressure; this antihypertensive effect apparently occurs via a ...

journal_title：Drug metabolism reviews

authors： Migdalof BH,Antonaccio MJ,McKinstry DN,Singhvi SM,Lan SJ,Egli P,Kripalani KJ

更新日期：1984-01-01 00:00:00

abstract：:The cannabinoid receptor 1 (CB1) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking behavior. Despite these benefits, development of orthosteric ther...

journal_title：Drug metabolism reviews

authors： Dopart R,Lu D,Lichtman AH,Kendall DA

更新日期：2018-02-01 00:00:00